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Therapeutic upregulation of DNA repair pathways: strategies and small molecule activators

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00673A, Review Article
Juhyung Song, Cheoljun Park, Francis E. B. Cabanting, Yong Woong Jun
Potential therapeutic target proteins for upregulating DNA repair system are reviewed, along with reported small-molecule activators.
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Correction: Anti-schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD90044H, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Kennosuke Itoh, Hiroki Nakahara, Atsushi Takashino, Aya Hara, Akiho Katsuno, Yuriko Abe, Takaaki Mizuguchi, Fumika Karaki, Shigeto Hirayama, Kenichiro Nagai, Reiko Seki, Noriko Sato, Kazuki Okuyama, Masashi Hashimoto, Ken Tokunaga, Hitoshi Ishida, Fusako Mikami, Kofi Dadzie Kwofie, Hayato Kawada, Bangzhong Lin, Kazuto Nunomura, Toshio Kanai, Takeshi Hatta, Naotoshi Tsuji, Junichi Haruta, Hideaki Fujii
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Human microbiome derived synthetic antimicrobial peptides with activity against Gram-negative, Gram-positive, and antibiotic resistant bacteria

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00383G, Research Article
Open Access
Walaa K. Mousa, Ashif Y. Shaikh, Rose Ghemrawi, Mohammed Aldulaimi, Aya Al Ali, Nour Sammani, Mostafa Khair, Mohamed I. Helal, Farah Al-Marzooq, Emilia Oueis
An AMP-derived short 15-mer peptide and its cyclic derivatives have low micromolar broad spectrum antibacterial activity, with rapid onset of bactericidal effect and a membrane-targeting mode of action.
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Amides of moronic acid and morolic acid with the tripeptides MAG and GAM targeting antimicrobial, antiviral and cytotoxic effects

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00742E, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Uladzimir Bildziukevich, Lucie Cerna, Jana Trylčová, Marie Kvasnicova, Lucie Rárová, David Šaman, Petra Lovecká, Jan Weber, Zdenek Wimmer
A series of amides of the selected plant triterpenoids, moronic acid and morolic acid, with the tripeptides MAG and GAM was designed and synthesized. Two required tripeptides 5 and 10...
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Continuous flow synthesis of N,N-dimethyltryptamine (DMT) analogues with therapeutic potential

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00562G, Research Article
Open Access
Andreas Simoens, Andreas Dejaegere, Marthe Vandevelde, Christian V. Stevens
Flow chemistry allows for the rapid and clean synthesis of therapeutically relevant tryptamines in good yields, including the large scale drug rizatriptan.
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Azo derivatives of monoterpenes as anti-Helicobacter pylori agents: from synthesis to structure-based target investigation

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00511B, Research Article
Open Access
Francesco Melfi, Marialuigia Fantacuzzi, Simone Carradori, Ilaria D'Agostino, Alessandra Ammazzalorso, Noemi Mencarelli, Marialucia Gallorini, Mattia Spano, Paolo Guglielmi, Mariangela Agamennone, Sazan Haji Ali, Ali Al-Samydai, Francesca Sisto
Monoterpene-derived azo benzenes showed selective antibacterial activity against Helicobacter pylori with a safe profile. An in silico investigation highlighted the inosine 5'-monophosphate dehydrogenase enzyme as the putative target.
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Medicinal chemistry-based perspective on thiophene and its derivatives: Exploring the structural insights to discover plausible druggable leads

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00450G, Review Article
Shikha Thakur, Devendra Kumar, shivani jaiswal, Kapil Kumar Goel, Pramod Rawat, Vivek Srivastava, Sonia Dhiman, Hemant R Jadhav, Ashish Ranjan Dwivedi
Thiophene is a privileged pharmacophore in medicinal chemistry owing to its diversified biological attributes. The thiophene moiety has been ranked 4th in US FDA drug approval of small drug molecules,...
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Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00579A, Research Article
Open Access
Cecilia C. Ayala-Aguilera, Yang Ge, Álvaro Lorente-Macías, Benjamin N. Jones, Catherine Adam, Neil O. Carragher, Asier Unciti-Broceta
A ligand-centred strategy combined with phenotypic screening was used to develop novel antiproliferative inhibitors against oesophageal cancer and identified a lead compound that induces potent anticancer activity and inhibits Aurora kinase A.
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Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00555D, Research Article
Shenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E. Tollefson, Karoly Toth, Peng Zhan, Xinyong Liu
The continuous mutational nature of SARS-CoV-2 and its inter-species' similarities emphasize the urgent need to design and develop more direct-acting antiviral agents against highly infectious variants.
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A novel approach for the synthesis of the cyclic lipopeptide globomycin

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00685B, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Samantha J. Bann, Stephen A. Cochrane
Lipid swapping: a new approach for the synthesis of globomycin that allows for facile lipid diversification.
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Synthesis, in silico and bio-evaluation studies of new isothiocyanate derivatives with respect to COX inhibition and H2S release profiles

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00495G, Research Article
Yakup Berkay Yilmaz, Tuğba Güngör, Serhat Dönmez, Hazal Nazlıcan Atalay, Pınar Siyah, Serdar Durdağı, Mehmet Ay, Tugba Boyunegmez Tumer
New isothiocyanate derivatives (I1–3 and I1a–e) were synthesized and screened for their anti-inflammatory activities and H2S-releasing capacities. Compounds I1 and I1c demonstrated the most potent and selective COX-2 inhibition.
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meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00601A, Research Article
Open Access
Brém Balázs, Bianca Stoean (Vasile), Éva Molnár, Eva Fischer-Fodor, Ovidiu Bălăcescu, Raluca Borlan, Monica Focsan, Adriana Grozav, Patriciu Achimaş-Cadariu, Emese Gál, Luiza Gaina
New meso-substituted AB3-type phenothiazinyl porphyrins and ferrocenylvinyl phenothiazinyl porphyrin were synthesised by Suzuki–Miyaura and Mizoroki–Heck cross-coupling reactions, respectively.
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Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00637B, Review Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Qiang Yang, Yunpeng Liu
Fc-glycan-specific ADC is a significant advance in site-specific ADCs for cancer therapy. Notably, JSKN003 and IBI343 have demonstrated promising results in phase 1 clinical trials and are advancing into phase 3 studies.
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Property-based optimisation of PROTACs

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00769G, Opinion
James Scott, Iacovos Michaelides, Markus Schade
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical...
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A practical guide for the assay-dependent characterisation of irreversible inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00707G, Review Article
Lavleen K. Mader, Jessica E. Borean, Jeffrey W. Keillor
Kinetic evaluations for assay dependent characterization of irreversible inhibitors.
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50 new primary health centres to be opened in State soon: Minister




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Agro-tourism push needs industry-specific policies, say farmers




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Paddy crop loss compensation pegged at ₹36,500




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Plea to include ‘panneer karumbu’ in Pongal gift hamper




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Urban Primary Health Centre stuck in cramped, temporary facility




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Property owners block the entrance to Balasubramanya temple in Karur




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Ernakulam Express to stop at Muthupettai during Kandhoori festival




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Tiruchi Corporation embarks on special drive at night to capture and sterilise street dogs

About 125 stray dogs have been caught and sterilised at Tiruchi animal birth control centres in the last 10 days after the Corporation launched the special drive




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HR&CE plans to bring properties around the Vennaimalai Temple under tenants list

The HR&CE department has cleared 34 properties around the Balasubramanyaswamy Temple at Vennaimalai in Karur district as per the High Court orders




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Tiruchi district SHGs compete to prepare healthy millet-based recipes at food festival

Women entrepreneurs urged to take advantage of social media platforms to advertise and market their products to a wider customer base




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Peravurani farmers’ market starts functioning




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‘State should retain primary agricultural cooperative societies under its purview’




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550: Sanity with Simen Svale Skogsrud and Espen Hovlandsdal

Simen and Espen from Sanity stop by to talk about the origins of Sanity, how Sanity Studio works, good use cases for Sanity, how Sanity does real time updates, what Groq is, and where to start with Sanity.




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553: TypeScript, DX, GripeScript, and Astro v2 with Fred Schott

Fred Schott stops by to talk about TypeScript, what DX means in 2023, a bit of GripeScript, and being transparent about what Astro is good at, and what it's not.




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561: Web Perf News, Web Sommelier, Data Analytics, and Passkeys

Topics for this one include how do you learn about web performance news? Do you need a web components sommelier? Our thoughts on Syntax going to Sentry, and being able to focus on the things you want to focus on. Passkeys, Arc split screen, and vibe driven development.




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567: Full Stack Dev, Load Bearing Developer, and Being Zod Curious

What do you do if your computer dies? Chris applies to work at Luro, Dave applies at CodePen, Dave's Zod curious, TypeScript, sorting out a 10MB blog post, and how much do you miss jQuery?




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572: Text Sqwunch Property, Figma Developer Mode, Stripe Elements

Show DescriptionDave reports back from the Figma Conference, how to build a better developer to designer bridge, do clients really want to update their website, using Stripe in 2023, permissions and sharing, and are you feeling overwhelmed by CSS in 2023? Listen on Website →Links Config 2023 | Figma’s Annual Conference Figma Visual Studio Code […]




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610: TypeScript in 2024, Signals, Productivity Sniped, and Follow Up

Dave's about to be eclipsed, the state of TypeScript in 2024, signals stage zero proposal, corrections on accessibility in frameworks (thanks!), web apps for better collaborative writing, getting productivity sniped, the problem with email may be you, indieweb follow up, and ultimate guitar tab apps.




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611: React! TypeScript! Jobification! Drupal!

Dave & Chris and thoughts on career advice that worked 3 years ago but isn't as helpful now, marking tests with ChatGPT, is taking a Drupal job in 2024 a good idea, Chris got #gear sniped, P3 color follow up, the confusing File System APIs, and where did all the lightboxes go?




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613: Recording Live Music, WebC, Open Source, & WordPress Studio

Chris bought recording gear off an Instagram ad, our thoughts on WebC, CodePen upgrades Yarn, thoughts on the commercial value of open source, Automattic releases an app to install WordPress locally, IBM buys Hashicorp, income tax software, and a hack for getting Safari to respect background colors used in a pseudo selector.




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637: Approachable Open Source with Brian Muenzenmeyer

Brian Muenzenmeyer joins the show to talk about his book, Approachable Open Source, ways we can make open source easier to get in, important conversations around funding and supporting open source, and whether money helps maintainers deal with burnout or not?




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The art of dispensing water

Water-ATMs are becoming the rage all over the country. A look at the mechanism.




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Typecasting eco-ideas

Important public buildings ignore the time-tested lessons of sustainability found in local architecture. By SATHYA PRAKASH VARANASHI




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Perez vs Lawson: A new F1 rivalry

RB driver Liam Lawson apologised to Sergio Perez after the pair clashed at the Mexican Grand Prix but the New Zealand rookie said he would not change his aggressive approach to Formula One racing.




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F1: Verstappen pulls off stunning win

Red Bull's Max Verstappen dealt Lando Norris a shattering blow in their Formula One title battle by winning a wet and chaotic Sao Paulo Grand Prix from 17th on the grid.




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Balrampur Chini hopes success of polylactic acid plant will be sweet

In conversation with Avantika Saraogi, ED, and Stefan Barot, President, Chemicals Division, Balrampur Chini Mills




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Superlative Class

The EQS SUV reinvigorates Mercedes-Benz’s game in the all-electric segment




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Unlocking renewable energy from industrial waste: Biogas production from spent wash

It is a sustainable solution for industrial waste management and renewable energy generation




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Brand expertise and heritage bubbling in a moka pot

Lessons from European brands that have won consumers’ mindspace for long years




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Why peer-to-peer lending has RBI on edge

Forced to drop many of its attractive features, peer-to-peer lending faces an existential crisis in India




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Keeping track of Scope-3 emissions from supply chains

Gurgaon-based startup OnlyGood FutureTech helps companies measure emissions generated by supply partners




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Planned meals, personal trainer, and a tea for every reason

Personal fitness diary




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Concussion: FIFA kicks off ‘suspect and protect’ drive 

Campaign raises awareness that concussion is a traumatic brain injury and a risk to every player on the pitch




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Can we escape the gas chamber we have walked into?

All countries are falling short of their promise to do their mite for climate action




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GalaxEye: A multi-sensor peek at earth from outer space

Startup sets out to fill a crucial gap in satellite imagery for real-world applications